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2-aminoindole compounds and methods for the treatment of malaria
专利权人:
PRESIDENT AND FELLOWS OF HARVARD COLLEGE;MASSACHUSETTS INSTITUTE OF TECHNOLOGY;GENZYME CORPORATION
发明人:
CORTESE, JOSEPH,MAZITSCHEK, RALPH,CLARDY, JON,WIRTH, DYANN,WIEGAND, ROGER,URGAONKAR, SAMEER,BANIECKI, MARY,CELATKA, CASSANDRA,XIANG, YIBIN,SKERLJ, RENATO,BOURQUE, ELYSE
申请号:
ES10827467
公开号:
ES2539365T3
申请日:
2010.10.28
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
A compound of formula IIa: ** Formula ** or a pharmaceutically acceptable salt thereof, in which: X is carbon or nitrogen; Y is carbon or nitrogen; R1a is hydrogen, halogen, nitro, cyano, hydroxy, (C1-C6) alkyl, (C1-C6) alkenyl, (C1-C6) alkynyl, (C1-C6) alkoxy, aryl, heteroaryl, cycloalkyl, heterocyclyl, arylalkyl ( C1-C3), heteroarylalkyl (C1-C3), cycloalkylalkyl (C1-C3), heterocyclylalkyl (C1-C3), hydroxyalkyl (C1-C3), N (R5a) 2, C (>; = NOH) NH2, NR5aCON (R5a ) 2, CON (R5a) 2, CO2R5a, COR6a, OC (O) R5a, SO2N (R5a) 2, SO2R6a, NR5aCOR6a, NR5aCO2R6a, NR5aSO2R6a or OC (>; = O) N (R5a) 2, each optionally substituted with one or more groups represented by R4a; R2a is (C1-C6) alkyl, (C1-C6) alkoxy, S-C1-C6 alkyl, SO-C1-C6 alkyl or SO2-C1-C6 alkyl, optionally substituted with one or more groups represented by R4a; R3a is halogen, (C1-C6) alkyl or (C1-C6) alkoxy, each optionally substituted with one or more groups represented by R4a; each R4a is independently halogen, nitro, cyano, hydroxy, (C1-C4) alkyl, halo (C1-C3) alkyl, hydroxyalkyl (C1-C4), alkoxy (C1-C4), haloalkoxy (C1-C4), aryl, haloaryl , cycloalkyl, arylalkyl (C1-C3), arylalkoxy (C1-C4), heterocyclyl, N (R5a) 2, C (>; = NOH) NH2, NR5aCON (R5a) 2, CON (R5a) 2, CO2R5a, COR6a, OC (O) R5a, SO2N (R5a) 2, SO2R6a, SR6a, S-(C1-C3) alkylcycloalkyl, NR5aCOR6a, NR5CO2R6a, NR5aSO2R6a, S (>; = O) R6a, -Ocycloalkyl, -O-heterocyclyl, ada OC (>; = O) N (R5a) 2, each R5a is independently hydrogen, (C1-C10) alkyl, aryl or aryl (C1-C6) alkyl, each optionally substituted with halogen, (C1-C3) alkoxy, alkyl ( C1-C3), haloalkyl (C1-C3), haloalkoxy (C1-C3), cyano or nitro; and each R6a is independently hydrogen, halogen, (C1-C10) alkyl, (C1-C10) alkoxy, (C1-C3) arylalkyl, cycloalkyl or (C1-C3) alkoxy, each optionally substituted with halogen, (C1-) alkoxy C3), (C1-C3) alkyl, (C1-C3) haloalkyl, (C1-C3) haloalkoxy, cyano or nitro.Un compuesto de fórmula IIa:**Fórmula** o una sal farmacéuticamente aceptable del mismo, en la qu
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